A novel nasal almotriptan loaded solid lipid nanoparticles in mucoadhesive in situ gel formulation for brain targeting: Preparation, characterization and in vivo evaluation

Triamcinolone acetonide (TA), an intermediate acting corticosteroid, is used in the treatment of posterior ocular diseases, such as inflammation, posterior uveitis, and diabetic macular edema. The objective of this investigation was to prepare TA-loaded solid lipid nanoparticles (TA-SLNs) and in situ gel (TA-SLN-IG) formulations for delivery into the deeper ocular tissues through the topical route. TA-SLNs were prepared by hot homogenization and ultrasonication method using glyceryl monostearate and Compritol® 888ATO as solid lipids and Tween®80 and Pluronic® F-68 as surfactants. TA-SLNs were optimized and converted to TA-SLN-IG by the inclusion of gellan gum and evaluated for their rheological properties. In vitro transcorneal permeability and in vivo ocular distribution of the TA-SLNs and TA-SLN-IG were studied using isolated rabbit corneas and New Zealand albino rabbits, respectively, and compared with TA suspension, used as control (TA-C). Particle size, PDI, zeta potential, assay, and entrapment efficiency of TA-SLNs were in the range of 200–350 nm, 0.3–0.45, −52.31 to −64.35 mV, 70–98%, and 97–99%, respectively. TA-SLN-IG with 0.3% gellan gum exhibited better rheological properties. The transcorneal permeability of TA-SLN and TA-SLN-IG was 10.2 and 9.3-folds higher compared to TA-C. TA-SLN-IG showed maximum tear concentration at 2 h, indicating an improved pre-corneal residence time, as well as higher concentrations in aqueous humor, vitreous humor and cornea at 6 h, suggesting sustained delivery of the drug into the anterior and posterior segment ocular tissues, when compared to TA-SLN and TA-C. The results, therefore, demonstrate that the lipid based nanoparticulate system combined with the in situ gelling agents can be a promising drug delivery platform for the deeper ocular tissues.

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Solid lipid nanoparticles for delivery of andrographolide across the blood-brain barrier: in vitro and in vivo evaluation

Colloids and Surfaces B Biointerfaces ◽

10.1016/j.colsurfb.2017.10.062 ◽

2018 ◽

Vol 161 ◽

pp. 302-313 ◽

Cited By ~ 33

Author(s):

Giulia Graverini ◽

Vieri Piazzini ◽

Elisa Landucci ◽

Daniela Pantano ◽

Pamela Nardiello ◽

...

Keyword(s):

Blood Brain Barrier ◽

Solid Lipid Nanoparticles ◽

Lipid Nanoparticles ◽

Brain Barrier ◽

In Vivo Evaluation ◽

Solid Lipid ◽

Blood Brain

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A comparative in vivo evaluation of anti-alzheimer activity of bacopa extract and its solid lipid nanoparticles

Current Bioactive Compounds ◽

10.2174/1573407216999201113121756 ◽

2020 ◽

Vol 16 ◽

Author(s):

Rajesh Kumar ◽

Rajeev Garg ◽

Navneet Khurana

Keyword(s):

Alzheimer’S Disease ◽

Alzheimer's Disease ◽

Solid Lipid Nanoparticles ◽

Extended Period ◽

Lipid Nanoparticles ◽

Nootropic Activity ◽

Active Constituent ◽

In Vivo Evaluation ◽

Solid Lipid

Purpose: Bacopa monnieri (Brahmi; family Scrophulariaceae) is a well-known plant known for its nootropic activity. Delivery of Bacosides (active constituent) is limited at the site of action owing to the existence of blood-brain barrier (BBB). In order to take the bacoside rich extract (BRE) across BBB, formulated solid lipid nanoparticles (SLNs) were used. Objective: The objective of this work was to evaluate the pharmacokinetic and pharmacodynamic behavior (in vivo potential) of the prepared SLNs containing BRE in comparison to BRE alone for the treatment of Alzheimer’s disease. Methods: Swiss albino male mice (25-30 gm) were used for the study. The pharmacokinetic as well as pharmacodynamic evaluation of formulated SLNs was performed in comparison to BRE in scopolamine-induced amnesia model. Results: BRE-loaded SLNs were found to be significantly more effective than BRE in alleviating the neurodegeneration. The pharmacokinetic study revealed the improved bioavailability of prepared SLNs with the potential of sustaining the drug release in mice for an extended period of time. Conclusion: The results demonstrated that the SLNs may be considered a potential delivery system for taking BRE across BBB to treat Alzheimer’s disease.

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